Cat. No.: HY-13532

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AS-252424

8 Cited Publications

Customer Review

Based on 8 publication(s) in Google Scholar

AS-252424 is a potent and selective PI3Kγ inhibitor with an IC₅₀ of 30±10 nM.

For research use only. We do not sell to patients.

Purity: 99.66%
CAS No.: 900515-16-4
Formula: C₁₄H₈FNO₄S
Molecular Weight:305.28

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AS-252424 Chemical Structure

CAS No.: 900515-16-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

AS-252424 is a potent and selective PI3Kγ inhibitor with an IC₅₀ of 30±10 nM.

IC₅₀ & Target^[1]

PI3Kγ

30 nM (IC₅₀)

PI3Kα

935 nM (IC₅₀)

PI3Kδ

20 μM (IC₅₀)

PI3Kβ

20 μM (IC₅₀)

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Monocyte	IC₅₀	53 μM Compound: 26	Inhibition of MCP1-induced chemotaxis of mouse primary monocytes Inhibition of MCP1-induced chemotaxis of mouse primary monocytes	[PMID: 16789742]
RAW264.7	IC₅₀	0.23 μM Compound: 26	Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage	[PMID: 16789742]
THP-1	IC₅₀	0.4 μM Compound: 26	Inhibition of MCP1-induced PKB/Akt phosphorylation in THP1 cells Inhibition of MCP1-induced PKB/Akt phosphorylation in THP1 cells	[PMID: 16789742]
THP-1	IC₅₀	4.73 μM Compound: 26	Inhibition of SCF1-induced PKB/Akt phosphorylation in THP1 cells Inhibition of SCF1-induced PKB/Akt phosphorylation in THP1 cells	[PMID: 16789742]
THP-1	IC₅₀	53 μM Compound: 26	Inhibition of MCP1-induced chemotaxis of THP1 cells Inhibition of MCP1-induced chemotaxis of THP1 cells	[PMID: 16789742]

In Vitro

AS-252424 also inhibits PI3Kα, PI3Kβ and PI3Kδ with IC₅₀s of 935±150 nM, 20 μM and 20 μM, respectively. AS-252424 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC₅₀ value of 52 μM, as well as in the monocytic cell line THP-1 with an IC₅₀ value of 53 μM. In the human monocytic cell line THP-1, MCP-1 binding to the GPCR chemokine receptor CCR2, strongly induces phosphorylation of PKB/Akt, which is effectively inhibited by AS-252424 at IC₅₀ values as low as 0.4 μM. In contrast, induction of PKB/Akt phosphorylation by colony stimulating factor (CSF-1), binding to the growth factor receptor c-fms, is only blocked by AS-252424 at IC₅₀ values as high as 4.7 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Oral administration of AS-252424 in a mouse model of acute peritonitis leads to a significant reduction of leukocyte recruitment. To evaluate the efficacy of AS-252424 to block leukocyte migration in vivo, it is tested in a mouse model of thioglycollate-induced peritonitis. Oral administration of AS-252424 at 10 mg/kg results in moderate reduction of neutrophil recruitment (35%±14%), almost matching the result observed in PI3Kγ-deficient mice. Given the short oral half-life of AS-252424 (t_1/2=1 h) and relative high clearance (2.25 L/kg per h), investigations at later time points (24-48 h) to assess macrophage and monoycyte recruitment are not undertaken. The modest pharmacokinetic properties do not appear to be caused by rapid oxidative metabolism (microsomal metabolism after 1 h: 16% (rat), 10% (human))^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 900515-16-4
Appearance Solid
Molecular Weight 305.28
Formula C₁₄H₈FNO₄S
Color Light yellow to brown
SMILES

O=C(NC/1=O)SC1=C/C2=CC=C(C3=CC=C(F)C=C3O)O2
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

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Journal Impact Factor

J Adv Res

The fatty acid receptor CD36 promotes macrophage infiltration via p110γ signaling to stimulate metastasis. [Abstract]

2025 Aug:74:237-253. PMID: 39419288
Cell Death Differ

PDK4-driven lactate accumulation facilitates LPCAT2 lactylation to exacerbate sepsis-induced acute lung injury. [Abstract]

2025 Oct 7. PMID: 41057687
Sci China Chem

2025 Jun 30.
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
J Mol Med (Berl)

PHP14 regulates hepatic stellate cells migration in liver fibrosis via mediating TGF-β1 signaling to PI3Kγ/AKT/Rac1 pathway. [Abstract]

2018 Feb;96(2):119-133. PMID: 29098317

AS-252424 purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2018 Feb;96(2):119-133. [Abstract]

The regulation of PHP14 on Akt phosphorylation is possibly via PI3Kγ in LX-2 cells. Cells are serum starvation 24 h, then treated TGF-β1 (10 ng/mL) 2 h, then added LY294002 (5 μM) or AS252424 (10 μM) as indicated; after another 2 h incubation, Western blot is performed to assess the protein expression of p-Akt.
J Biol Chem

The mTOR inhibitor manassantin B reveals a crucial role of mTORC2 signaling in Epstein-Barr virus reactivation. [Abstract]

2020 May 22;295(21):7431-7441. PMID: 32312752
bioRxiv

2026 May 7.
Biomed Pharmacother

Lutein attenuates rhabdomyolysis-induced acute kidney injury by inhibiting ACSL4-mediated ferroptosis. [Abstract]

2025 Jul:188:118222. PMID: 40460552

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (81.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2757 mL

16.3784 mL

32.7568 mL

5 mM

0.6551 mL

3.2757 mL

6.5514 mL

10 mM

0.3276 mL

1.6378 mL

3.2757 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration Concentration

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Molecular Weight Molecular Weight

Dilution Calculator

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Protocol

Kinase Assay^[1]

A PI3Kγ lipid kinase assay, based on the neomycin-coated scintillation proximity assay (SPA) bead technology, is performed in 384-well plates using ATP/[γ³³P]ATP and PtdIns. Kinase assays for IC₅₀ value determinations with PI3Kα, PI3Kβ, and PI3Kδ are carried out^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

After 3 h of starvation in serum-free medium, Raw-264 macrophages are pretreated with inhibitors (e.g., AS-252424, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM and 100 μM) or DMSO for 30 min and stimulated for 5 min with 50 nM C5a. PKB/Akt phosphorylation is monitored using phospho-Ser-473 Akt specific antibody and standard ELISA protocols^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
PI3Kγ knockout (KO) mice are used. Oral administration of AS-252424 at 10 mg/kg is performed in PI3Kγ-deficient mice.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Pomel V, et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. J Med Chem. 2006 Jun 29;49(13):3857-71. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2757 mL	16.3784 mL	32.7568 mL	81.8920 mL
	5 mM	0.6551 mL	3.2757 mL	6.5514 mL	16.3784 mL
	10 mM	0.3276 mL	1.6378 mL	3.2757 mL	8.1892 mL
	15 mM	0.2184 mL	1.0919 mL	2.1838 mL	5.4595 mL
	20 mM	0.1638 mL	0.8189 mL	1.6378 mL	4.0946 mL
	25 mM	0.1310 mL	0.6551 mL	1.3103 mL	3.2757 mL
	30 mM	0.1092 mL	0.5459 mL	1.0919 mL	2.7297 mL
	40 mM	0.0819 mL	0.4095 mL	0.8189 mL	2.0473 mL
	50 mM	0.0655 mL	0.3276 mL	0.6551 mL	1.6378 mL
	60 mM	0.0546 mL	0.2730 mL	0.5459 mL	1.3649 mL
	80 mM	0.0409 mL	0.2047 mL	0.4095 mL	1.0237 mL

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AS-252424

Covalent Screening Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) AS-252424

All PI3K Isoforms

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

AS-252424 Related Classifications

HY-13532 Related Classifications